Molecular Formula | C21H21F3IN3O2
|
Molar Mass | 531.31 |
Density | 1.706 |
Melting Point | 165 - 166°C |
Boling Point | 565.9±50.0 °C(Predicted) |
Solubility | Chloroform (Slightly), DMSO (Slightly), Ethyl Acetate (Slightly), Methanol (Slig |
Appearance | Solid |
Color | Off-White |
pKa | 13.13±0.20(Predicted) |
Storage Condition | Refrigerator |
In vitro study | Cobimetinib exhibits strong inhibitory activity against the growth of a broad group of tumor cells, particularly against BRAF or KRAS mutant cancer cell lines. Binding of GDC-0941,GDC-0973 in 888MEL and A2058 cells resulted in decreased viability, pathway inhibition, and increased apoptosis. Co-administration of GDC-0973 and vemurafenib significantly increased decreased GLUT-1 levels on cell membranes in all BRAF V600E lines. |
In vivo study | Cobimetinib (10 mg/kg, p.o.) produced anti-tumor effects in mice bearing BRAF V600E and KRAS mutant tumors, which combined GDC-0973 and GDC-0941 to improve efficacy. Binding of GDC-0973 to GDC-0941 induced reduced levels of hexokinase II,c-RAF,Ksr and p-MEK proteins in drug-resistant loading A375 xenograft mice. |